Low density lipoprotein cholesterin (LCL-C) level of plasma is closely related to the occurrence of cardiovascular diseases risk, and the low density lipoprotein receptor (LDL-R) expressed on liver cell surface is one key factor deciding the level of LDL-C. The PCSK9 in blood can specifically bind to LDL-R on cell surface to form complex compound which is transferred to lysosome and accelerate the degradation of LDL-R, and increase the level of LDL-C. Numerous basic researches and clinical trial results show that removal of low density lipoprotein (LDL) in plasma can be accelerated after exogenous interventions inhibit the activity of PCSK9 thus to have a good lipid-lowering effect. Therefore, PCSK9 inhibitor will be probably a new generation of drugs for the treatment of dyslipidemia and relevant cardiovascular diseases.
The following chemical compound PF-06446846 and similar chemical compounds are reported in WO2014170786.
